تفاعل #9978

معادلة التفاعل

4-bromo-2-(4-fluorophenyl)-3-(pyridin-4-yl)thiophene

3-bromo-5-(4-fluorophenyl)-4-(pyridin-4-yl)pyrazole

(S)-1,2,3,5,6,7,8,8a-octahydroindolizin-7-one

→

title compound

المردود 23.0%

(S)-2-(4-Fluorophenyl)-4-(1,2,3,5,8,8a-hexahydroindolizin-7-yl)-3-(pyridin-4-yl)thiophene

المردود 23.0%

ظروف التفاعل

المعالجة

1. 1
   أخرىprepared
2. 2
   أخرىthe resulting product was subjected to a dehydration reaction
3. 3
   workup.ADDITIONtreated by column chromatography through silica gel (eluent, ethyl acetate:methanol:isopropylamine=10:10:1)

الإجراء التجريبي

Following a procedure similar to that described in Example 2-2), but using 4-bromo-2-(4-fluorophenyl)-3-(pyridin-4-yl)thiophene prepared as described in 5) instead of 3-bromo-5-(4-fluorophenyl)-4-(pyridin-4-yl)pyrazole, and using (S)-1,2,3,5,6,7,8,8a-octahydroindolizin-7-one instead of (±)-1,2,3,5,6,7,8,8a-octahydroindolizin-7-one, the resulting product was subjected to a dehydration reaction as described in Example 3 and then treated by column chromatography through silica gel (eluent, ethyl acetate:methanol:isopropylamine=10:10:1), to give the title compound (Rf=0.50, 263 mg) as a brown amorphous solid (yield 23%).

المصدر